EA030431B1 - РЕГУЛЯТОРЫ Nrf2 - Google Patents

РЕГУЛЯТОРЫ Nrf2 Download PDF

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Publication number
EA030431B1
EA030431B1 EA201691259A EA201691259A EA030431B1 EA 030431 B1 EA030431 B1 EA 030431B1 EA 201691259 A EA201691259 A EA 201691259A EA 201691259 A EA201691259 A EA 201691259A EA 030431 B1 EA030431 B1 EA 030431B1
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EA
Eurasian Patent Office
Prior art keywords
methyl
benzo
dioxido
phenyl
dihydro
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EA201691259A
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English (en)
Russian (ru)
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EA201691259A1 (ru
Inventor
Джеффри Чарльз Боэм
Томас Гленмор Дэвис
Элисон Джо-Энн Вулфорд
Шарлотт Мэри Гриффитс-Джоунз
Хендрика Мария Герарда Виллемс
Дэвид Нортон
Гордон Саксти
Томас Дэниел Хейтман
Тинди Ли
Джеффри К. Кернс
Родерик С. Дэвис
Хунсин Янь
Original Assignee
Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
Астекс Терапьютикс Лимитед
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Publication of EA201691259A1 publication Critical patent/EA201691259A1/ru
Publication of EA030431B1 publication Critical patent/EA030431B1/ru

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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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    • C07D281/02—Seven-membered rings
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/04—Ortho-condensed systems
EA201691259A 2013-12-18 2014-12-17 РЕГУЛЯТОРЫ Nrf2 EA030431B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361917466P 2013-12-18 2013-12-18
US201461980091P 2014-04-16 2014-04-16
PCT/IB2014/067027 WO2015092713A1 (en) 2013-12-18 2014-12-17 Nrf2 regulators

Publications (2)

Publication Number Publication Date
EA201691259A1 EA201691259A1 (ru) 2016-11-30
EA030431B1 true EA030431B1 (ru) 2018-08-31

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US (2) US10144731B2 (es)
EP (1) EP3083614B1 (es)
JP (1) JP6630671B2 (es)
KR (1) KR102301867B1 (es)
CN (1) CN105829305B (es)
AU (2) AU2014369153B2 (es)
BR (1) BR112016014180A2 (es)
CA (1) CA2934216C (es)
CL (1) CL2016001516A1 (es)
CR (1) CR20160272A (es)
DO (1) DOP2016000145A (es)
EA (1) EA030431B1 (es)
ES (1) ES2784244T3 (es)
IL (1) IL245727B (es)
MX (1) MX370410B (es)
PE (1) PE20160901A1 (es)
PH (1) PH12016501151A1 (es)
SG (1) SG11201604611SA (es)
WO (1) WO2015092713A1 (es)

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WO2016203401A1 (en) 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
JP2018517732A (ja) * 2015-06-15 2018-07-05 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎｒｆ２レギュレーター
WO2017060854A1 (en) * 2015-10-06 2017-04-13 Glaxosmithkline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
EP3371167A1 (en) * 2015-10-06 2018-09-12 GlaxoSmithKline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as nrf2 regulators
CN105566241B (zh) * 2016-01-18 2018-05-25 中国药科大学 1-磺酰胺基-4-芳氧基类化合物、制备方法及其医药用途
ES2846886T3 (es) 2016-02-03 2021-07-30 Rigel Pharmaceuticals Inc Compuestos activadores de Nrf2 y usos de los mismos
WO2018104766A1 (en) * 2016-12-06 2018-06-14 Glaxosmithkline Intellectual Property Development Limited 3-(2,3-dihydro-1h-inden-5-yl)propanoic acid derivatives and their use as nrf2 regulators
WO2018109642A1 (en) * 2016-12-12 2018-06-21 Glaxosmithkline Intellectual Property Development Limited N-aryl pyrazoles as nrf2 regulators
US20200031820A1 (en) * 2016-12-12 2020-01-30 Glsxosmithkline Intellectual Property Development Limited 3-carboxylic acid pyrroles as nrf2 regulators
US11117905B2 (en) 2016-12-14 2021-09-14 Glaxosmithkline Intellectual Property Development Limited Bisaryl heterocycles as NRF2 activators
EP3555088B1 (en) 2016-12-14 2021-11-24 GlaxoSmithKline Intellectual Property Development Limited Bisaryl amides as nrf2 regulators
WO2018109648A1 (en) * 2016-12-14 2018-06-21 Glaxosmithkline Intellectual Property Development Limited 3-oxo-1,4-diazepinyle compounds as nrf2 activators
BR112019012300A2 (pt) 2016-12-15 2019-11-12 Glaxosmithkline Ip Dev Ltd ativadores nrf2
WO2018109649A1 (en) * 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Ether linked triazoles as nrf2 regulators
US10786471B2 (en) 2017-02-06 2020-09-29 Massachusetts Institute Of Technology Methods and products related to glutaminase inhibitors
JP2020097526A (ja) * 2017-03-28 2020-06-25 武田薬品工業株式会社 複素環化合物
WO2019116231A1 (en) 2017-12-11 2019-06-20 Glaxosmithkline Intellectual Property Development Limited Nrf2 activator for the treatment of acute lung injury, acute respiratory distress syndrome and multiple organ dysfunction syndrome
EP3723764A1 (en) * 2017-12-11 2020-10-21 GlaxoSmithKline Intellectual Property Development Ltd Nrf2 activator for the treatment of acute lung injury, acute respiratory distress syndrome and multiple organ dysfunction syndrome
US11643407B2 (en) 2018-05-23 2023-05-09 Glaxosmithkline Intellectual Property Development Limited Indanes as NRF2 activators
WO2020018788A1 (en) * 2018-07-20 2020-01-23 Dana-Farber Cancer Institute, Inc. Degraders that target proteins via keap1
PT3833662T (pt) * 2018-08-20 2024-03-18 Janssen Pharmaceutica Nv Inibidores da interação proteína-proteína keap1-nrf2
MX2021006527A (es) * 2018-12-05 2021-07-21 Scohia Pharma Inc Compuesto macrociclico y su uso.
MX2021009659A (es) 2019-02-15 2021-09-08 Glaxosmithkline Ip Dev Ltd Hidroxipiridoxazepinas como activadores de nrf2.
US20220177466A1 (en) * 2019-04-08 2022-06-09 Dana-Farber Cancer Institute, Inc. Degraders of kelch-like ech-associated protein 1 (keap1)
US20220259223A1 (en) 2019-05-31 2022-08-18 Ube Industries, Ltd. Benzotriazole derivative
JPWO2021002473A1 (es) * 2019-07-03 2021-01-07
WO2021170774A1 (en) 2020-02-28 2021-09-02 Les Laboratoires Servier New macrocyclic compounds, a process for their preparation and pharmaceutical compositions containing them
KR20230127268A (ko) 2020-12-28 2023-08-31 센주 세이야꾸 가부시키가이샤 Nrf2 활성화 화합물
WO2023210741A1 (ja) * 2022-04-28 2023-11-02 第一三共株式会社 ベンゾトリアゾール化合物
CN117603075B (zh) * 2024-01-18 2024-04-12 深圳创元生物医药科技有限公司 一种碳13标记的3-羧酸苯丙氨酸的制备方法

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